2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
CAS NO.：2237942-08-2 Product Name：MC180295 Synonyms：MC180295;[4-Amino-2-[[(2R)-2-bicyclo[2.2.1]heptanyl]amino]-1,3-thiazol-5-yl]-(2-nitrophenyl)methanone;(rel)-MC180295 EINECS: Molecular Formula：C17H18N4O3S Molecular Weight：358.416
Target:
In Vivo
(rel)-MC180295 (MC180295; 20 mg/kg, i.p., qod) inhibtis significant anti-tumor activity in mice bearing SW48 cells, shows no inhibitory activity against human T cell growth in vivo[1].
In Vitro
(rel)-MC180295 (MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs, such as CDK1-Cyclin B (IC50, 138 nM), CDK2-Cyclin A (IC50, 233 nM), CDK2-Cyclin E (IC50, 367 nM), CDK3-Cyclin E (IC50, 399 nM), CDK4-Cyclin D (IC50, 112 nM), CDK5-P35 (IC50, 159 nM), CDK5-P25 (IC50, 186 nM), CDK6-Cyclin D3 (IC50, 712 nM), and CDK7-CycH/MAT1 (IC50, 555 nM). (rel)-MC180295 also inhibits GSK-3α and GSK-3β[1]. (rel)-MC180295 (500 nM) reactivates epigenetically silenced genes by targeting CDK9 without affecting DNA methylation[1]. (rel)-MC180295 (0.1 μM) inhibits the proliferation in cancer cells[1].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Zhang H, et al. Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer. Cell. 2018 Nov 15;175(5):1244-1258.e26.
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